KB-R7943 mesylate | CAS#182004-65-5 | reverse Na(+)/Ca(2+) exchanger inhibitor

MedKoo Cat#: 522400 | Name: KB-R7943 mesylate

Description:

WARNING: This product is for research use only, not for human or veterinary use.

KB-R7943 is a potent, selective inhibitor of the reverse mode of the Na+/Ca2+ exchanger (IC50 = 0.7 μM). KB-R7943 does not modify secondary pathology in the thalamus following focal cerebral stroke in rats. KB-R7943 blocks opening of the mitochondrial permeability transition pore. KB-R7943 restores endothelium-dependent relaxation induced by advanced glycosylation end products in rat aorta. KB-R7943 inhibits high glucose-induced endothelial ICAM-1 expression and monocyte-endothelial adhesion.

Chemical Structure

KB-R7943 mesylate

CAS#182004-65-5 (mesylate)

Theoretical Analysis

MedKoo Cat#: 522400

Name: KB-R7943 mesylate

CAS#: 182004-65-5 (mesylate)

Chemical Formula: C17H21N3O6S2

Exact Mass: 427.0872

Molecular Weight: 427.49

Elemental Analysis: C, 47.76; H, 4.95; N, 9.83; O, 22.46; S, 15.00

Price and Availability

Size	Price	Availability
25mg	USD 150.00	Ready to ship
50mg	USD 250.00	Ready to ship
100mg	USD 450.00	Ready to ship
200mg	USD 750.00	Ready to ship
500mg	USD 1,350.00	Ready to ship
1g	USD 2,350.00	Ready to ship
2g	USD 4,350.00	Ready to ship

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Related CAS #

182004-64-4 (free base) 182004-65-5 (mesylate)

Synonym

KB-R7943; KB R7943; KB-R 7943; KB-R7943 mesylate

IUPAC/Chemical Name

2-[2-[4-(4-Nitrobenzyloxy)phenyl]ethyl]isothiourea mesylate

InChi Key

WGIKEBHIKKWJLG-UHFFFAOYSA-N

InChi Code

InChI=1S/C16H17N3O3S.CH4O3S/c17-16(18)23-10-9-12-3-7-15(8-4-12)22-11-13-1-5-14(6-2-13)19(20)21;1-5(2,3)4/h1-8H,9-11H2,(H3,17,18);1H3,(H,2,3,4)

SMILES Code

N=C(N)SCCC1=CC=C(OCC2=CC=C([N+]([O-])=O)C=C2)C=C1.OS(=O)(C)=O

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#BBC50930

QC Data

View QC data: current batch, Lot#BBC50930

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

KB-R7943 mesylate is a widely used inhibitor of the reverse Na+/Ca2+ exchanger (NCX(rev)) with IC50 of 5.7 μM.

In vitro activity:

The effect of KB-R7943, an inhibitor of the plasmalemmal Na+-Ca2+ exchanger, on mitochondrial Ca2+ transporters was examined with membrane-permeabilized cardiomyocyte-derived H9c2 cells expressing the fluorescent Ca2+ indicator, yellow cameleon 3.1, in the mitochondria. KB-R7943, as well as ruthenium red, inhibited the rise in mitochondrial Ca2+ on increasing the extramitochondrial Ca2+ concentration from 0 nM to 300 nM. CGP-37157, but not KB-R7943, inhibited the decline in mitochondrial Ca2+on return to Ca2+ free extramitochondrial solution. These results indicated that KB-R7943 has inhibitory effects on the mitochondrial Ca2+ uniporter, but not on the mitochondrial Na+-Ca2+ exchanger. Reference: Biol Pharm Bull. 2020 Dec 1;43(12):1993-1996. https://dx.doi.org/10.1248/bpb.b20-00747

In vivo activity:

To confirm that KB-R7943 had the same effect in vivo, PC3 cells were subcutaneously injected into male nude mice. KB-R7943 inhibited the growth of tumors resulting from PC3 cell xenografts (Figure 6A). More importantly, Ki-67 levels decreased and LC3 and caspase 3 levels increased (Figure 6B), indicating that KB-R7943 inhibited tumor growth by inducing autophagosome accumulation and apoptosis. Reference: Oncotarget. 2016 Jul 5;7(27):42059-42070. https://www.ncbi.nlm.nih.gov/pmc/articles/pmid/27275542/

	Solvent	mg/mL	mM
Solubility
	DMSO	27.0	63.16

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 427.49 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

In vitro protocol:

1. Namekata I, Odaka R, Hamaguchi S, Tanaka H. KB-R7943 Inhibits the Mitochondrial Ca2+ Uniporter but Not Na+-Ca2+ Exchanger in Cardiomyocyte-Derived H9c2 Cells. Biol Pharm Bull. 2020 Dec 1;43(12):1993-1996. doi: 10.1248/bpb.b20-00747. Epub 2020 Oct 6. PMID: 33028749. 2. Long Z, Chen B, Liu Q, Zhao J, Yang Z, Dong X, Xia L, Huang S, Hu X, Song B, Li L. The reverse-mode NCX1 activity inhibitor KB-R7943 promotes prostate cancer cell death by activating the JNK pathway and blocking autophagic flux. Oncotarget. 2016 Jul 5;7(27):42059-42070. doi: 10.18632/oncotarget.9806. PMID: 27275542; PMCID: PMC5173116.

In vivo protocol:

1. Long Z, Chen B, Liu Q, Zhao J, Yang Z, Dong X, Xia L, Huang S, Hu X, Song B, Li L. The reverse-mode NCX1 activity inhibitor KB-R7943 promotes prostate cancer cell death by activating the JNK pathway and blocking autophagic flux. Oncotarget. 2016 Jul 5;7(27):42059-42070. doi: 10.18632/oncotarget.9806. PMID: 27275542; PMCID: PMC5173116. 2. Su Y, Mao N, Li M, Dong X, Lin FZ, Xu Y, Li YB. KB-R7943 restores endothelium-dependent relaxation induced by advanced glycosylation end products in rat aorta. J Diabetes Complications. 2013 Jan-Feb;27(1):6-10. doi: 10.1016/j.jdiacomp.2012.08.007. Epub 2012 Sep 27. PMID: 23021774.

1: Chang PC, Wo HT, Lee HL, Wen MS, Chou CC. Paradoxical effects of KB-R7943 on arrhythmogenicity in a chronic myocardial infarction rabbit model. J Cardiol. 2015 Jul;66(1):80-7. doi: 10.1016/j.jjcc.2014.08.002. Epub 2014 Sep 16. PubMed PMID: 25241015. 2: Lipsanen A, Parkkinen S, Khabbal J, Mäkinen P, Peräniemi S, Hiltunen M, Jolkkonen J. KB-R7943, an inhibitor of the reverse Na(+)/Ca(2+) exchanger, does not modify secondary pathology in the thalamus following focal cerebral stroke in rats. Neurosci Lett. 2014 Sep 19;580:173-7. doi: 10.1016/j.neulet.2014.08.003. Epub 2014 Aug 12. PubMed PMID: 25123443. 3: Abramochkin DV, Vornanen M. Inhibition of the cardiac ATP-dependent potassium current by KB-R7943. Comp Biochem Physiol A Mol Integr Physiol. 2014 Sep;175:38-45. doi: 10.1016/j.cbpa.2014.05.005. Epub 2014 May 17. PubMed PMID: 24845199. 4: Ren Y, Deng L, Cai Y, Lv Y, Jia D. The protective effect of Na+/Ca2+ exchange blocker kb-r7943 on myocardial ischemia-reperfusion injury in hypercholesterolemic rat. Cell Biochem Biophys. 2014 Nov;70(2):1017-22. doi: 10.1007/s12013-014-0012-7. PubMed PMID: 24840224. 5: Re: Yamashita J, Itoh M, Kuro T, Kobayashi Y, Ogata M, Takaoka m, and Matsumura Y (2001) pre- or post-ischemic treatment with a novel na+/ca2+ exchange inhibitor, kb-r7943, shows renal protective effects in rats with ischemic acute renal failure. J pharmacol exp ther 296:412-419. J Pharmacol Exp Ther. 2014 May;349(2):344. doi: 10.1124/jpet.114.05er14. PubMed PMID: 24713231. 6: Wiczer BM, Marcu R, Hawkins BJ. KB-R7943, a plasma membrane Na(+)/Ca(2+) exchanger inhibitor, blocks opening of the mitochondrial permeability transition pore. Biochem Biophys Res Commun. 2014 Jan 31;444(1):44-9. doi: 10.1016/j.bbrc.2014.01.009. Epub 2014 Jan 14. PubMed PMID: 24434143; PubMed Central PMCID: PMC3951502. 7: Abramochkin DV, Alekseeva EI, Vornanen M. Inhibition of the cardiac inward rectifier potassium currents by KB-R7943. Comp Biochem Physiol C Toxicol Pharmacol. 2013 Sep;158(3):181-6. doi: 10.1016/j.cbpc.2013.08.001. Epub 2013 Aug 22. PubMed PMID: 23973826. 8: Yang D, Yang D, Jia R, Tan J. Na+/Ca2+ exchange inhibitor, KB-R7943, attenuates contrast-induced acute kidney injury. J Nephrol. 2013 Sep-Oct;26(5):877-85. doi: 10.5301/jn.5000259. Epub 2013 Mar 5. PubMed PMID: 23475466. 9: Lv Y, Ren Y, Sun L, Wang S, Wei M, Jia D. Protective effect of Na(+)/Ca (2+) exchange blocker KB-R7943 on myocardial ischemia-reperfusion injury in hypercholesterolemic rats. Cell Biochem Biophys. 2013 Jun;66(2):357-63. doi: 10.1007/s12013-012-9474-7. PubMed PMID: 23212178. 10: Su Y, Mao N, Li M, Dong X, Lin FZ, Xu Y, Li YB. KB-R7943 restores endothelium-dependent relaxation induced by advanced glycosylation end products in rat aorta. J Diabetes Complications. 2013 Jan-Feb;27(1):6-10. doi: 10.1016/j.jdiacomp.2012.08.007. Epub 2012 Sep 27. PubMed PMID: 23021774. 11: Ren Y, Cai Y, Jia D. Comparative antiapoptotic effects of KB-R7943 and ischemic postconditioning during myocardial ischemia reperfusion. Cell Biochem Biophys. 2012 Nov;64(2):137-45. doi: 10.1007/s12013-012-9382-x. PubMed PMID: 22707298. 12: Cheng H, Zhang Y, Du C, Dempsey CE, Hancox JC. High potency inhibition of hERG potassium channels by the sodium-calcium exchange inhibitor KB-R7943. Br J Pharmacol. 2012 Apr;165(7):2260-73. doi: 10.1111/j.1476-5381.2011.01688.x. PubMed PMID: 21950687; PubMed Central PMCID: PMC3413861. 13: Cheng H, Smith GL, Hancox JC, Orchard CH. Inhibition of spontaneous activity of rabbit atrioventricular node cells by KB-R7943 and inhibitors of sarcoplasmic reticulum Ca(2+) ATPase. Cell Calcium. 2011 Jan;49(1):56-65. doi: 10.1016/j.ceca.2010.11.008. Epub 2010 Dec 15. PubMed PMID: 21163524; PubMed Central PMCID: PMC3048929. 14: Jia D. The protective effect of mitochondrial ATP-sensitive K+ channel opener, nicorandil, combined with Na+/Ca2+ exchange blocker KB-R7943 on myocardial ischemia-reperfusion injury in rat. Cell Biochem Biophys. 2011 Jul;60(3):219-24. doi: 10.1007/s12013-010-9142-8. PubMed PMID: 21132540. 15: Brustovetsky T, Brittain MK, Sheets PL, Cummins TR, Pinelis V, Brustovetsky N. KB-R7943, an inhibitor of the reverse Na+ /Ca2+ exchanger, blocks N-methyl-D-aspartate receptor and inhibits mitochondrial complex I. Br J Pharmacol. 2011 Jan;162(1):255-70. doi: 10.1111/j.1476-5381.2010.01054.x. PubMed PMID: 20883473; PubMed Central PMCID: PMC3012420. 16: Tashiro M, Inoue H, Konishi M. KB-R7943 inhibits Na+-dependent Mg2+ efflux in rat ventricular myocytes. J Physiol Sci. 2010 Nov;60(6):415-24. doi: 10.1007/s12576-010-0113-z. Epub 2010 Sep 23. PubMed PMID: 20862573. 17: Algara-Suárez P, Mejía-Elizondo R, Sims SM, Saavedra-Alanis VM, Espinosa-Tanguma R. The 1.3 isoform of Na+-Ca 2+ exchanger expressed in guinea pig tracheal smooth muscle is less sensitive to KB-R7943. J Physiol Biochem. 2010 Jun;66(2):117-25. doi: 10.1007/s13105-010-0016-8. Epub 2010 Apr 29. PubMed PMID: 20428991. 18: Condrescu M, Reeves JP. Inhibition of sodium-calcium exchange by KB-R7943: Dodecylamine and sphingosine in transfected Chinese hamster ovary cells. Cell Calcium. 2010 May;47(5):404-11. doi: 10.1016/j.ceca.2010.02.004. Epub 2010 Mar 5. PubMed PMID: 20206994. 19: Li J, Jin HB, Sun YM, Su Y, Wang LF. KB-R7943 inhibits high glucose-induced endothelial ICAM-1 expression and monocyte-endothelial adhesion. Biochem Biophys Res Commun. 2010 Feb 19;392(4):516-9. doi: 10.1016/j.bbrc.2009.12.183. Epub 2010 Jan 22. PubMed PMID: 20096662. 20: Storozhevykh TP, Senilova YE, Brustovetsky T, Pinelis VG, Brustovetsky N. Neuroprotective effect of KB-R7943 against glutamate excitotoxicity is related to mild mitochondrial depolarization. Neurochem Res. 2010 Feb;35(2):323-35. doi: 10.1007/s11064-009-0058-x. Epub 2009 Sep 22. PubMed PMID: 19771515.